1,720,997 research outputs found
Screening of in vitro and in silico α-amylase, α-glucosidase, and lipase inhibitory activity of oxyprenylated natural compounds and semisynthetic derivatives
No full textFaraone, Immacolata, Russo, Daniela, Genovese, Salvatore, Milella, Luigi, Monn, Magnus, e, Epifano, Francesco, Fiorito, Serena (2021): Screening of in vitro and in silico α-amylase, α-glucosidase, and lipase inhibitory activity of oxyprenylated natural compounds and semisynthetic derivatives. Phytochemistry (112781) 187: 1-10, DOI: 10.1016/j.phytochem.2021.112781, URL: http://dx.doi.org/10.1016/j.phytochem.2021.11278
Fig. 5. G in The healing bitterness of Gentiana lutea L., phytochemistry and biological activities: A systematic review
No full textFig. 5. G. lutea extract and its constituents could inhibit vascular smooth muscle cells proliferation acting downstream of PDGF-receptor but upstream ERK1/2 leading to the slackening of the atherosclerotic process. At the same time, amarogentin could inhibit MAPKs and PLCγ activation avoiding platelet activation.Published as part of Ponticelli, Maria, Lela, Ludovica, Moles, Mariapia, Mangieri, Claudia, Bisaccia, Donatella, Faraone, Immacolata, Falabella, Roberto & Milella, Luigi, 2023, The healing bitterness of Gentiana lutea L., phytochemistry and biological activities: A systematic review, pp. 1-27 in Phytochemistry (113518) 206 on page 13, DOI: 10.1016/j.phytochem.2022.113518, http://zenodo.org/record/823001
Fig. 3 in Screening of in vitro and in silico α-amylase, α-glucosidase, and lipase inhibitory activity of oxyprenylated natural compounds and semisynthetic derivatives
No full textFig. 3. Docking of compounds 3, 9, 11, and 15 in human α-amylase and α-glucosidase enzymes. The original structures of α-amylase (1XD0) and α-glucosidase (3TOP) enzymes contain the inhibitor acarbose (carbons coloured in orange and hexoses numbered in A and F, respectively). The docking results in α-amylase (B-E, light grey surface) and α-glucosidase (G-J, beige) enzymes with compounds 3 (pink, B and G), 9 (cyan, C and H), 11 (magenta, D and I), and 15 (green, E and J) are shown with their respective binding energies. The carbons of the residues lining the binding pocket are coloured in white, with the active site residues in yellow (R210, D212, E248, and R352 in α-amylase; D1420, E1423, and D1526 in α-glucosidase enzyme). Residues making hydrogen bonds with the ligands are indicated (B- E and G-J). (For interpretation of the references to colour in this figure legend, the reader is referred to the Web version of this article.)Published as part of Faraone, Immacolata, Russo, Daniela, Genovese, Salvatore, Milella, Luigi, Monn, Magnus, e, Epifano, Francesco & Fiorito, Serena, 2021, Screening of in vitro and in silico α-amylase, α-glucosidase, and lipase inhibitory activity of oxyprenylated natural compounds and semisynthetic derivatives, pp. 1-10 in Phytochemistry (112781) 187 on page 6, DOI: 10.1016/j.phytochem.2021.112781, http://zenodo.org/record/825875
Insight into the Interaction of Humulus lupulus L. Specialized Metabolites and Gastrointestinal Bitter Taste Receptors: In Vitro Study in STC-1 Cells and Molecular Docking
Full text link: Bitter taste receptors, also known as taste 2 receptors (T2R), are expressed throughout the body and are involved in regulating different physiological processes. T2R expression in the intestinal tract regulates orexigenic and anorexigenic peptide secretion, thus becoming potential a potential target for controlling food intake and the prevalence of obesity and overweight. The present study aims to investigate the implication of hop bitter compounds such as α-acids, β-acids, and xanthohumol in the secretion of anorexigenic hormones and T2R expression in intestinal STC-1 cells. The tested bitter compounds induced the secretion of the anorexigenic hormones glucagon-like peptide 1 and cholecystokinin concurrently with a selective increase of murine Tas2r expression. Xanthohumol and α-acids selectively increase Tas2r138 and Tas2r130-Tas2r138 expression, respectively, in STC-1 cells, while β-acids increased the expression of all bitter receptors studied, including Tas2r119, Tas2r105, Tas2r138, Tas2r120, and Tas2r130. Increased intracellular calcium levels confirmed this activity. As all investigated bitter molecules increased Tas2r138 expression, computational studies were performed on Tas2r138 and its human orthologue T2R38 for the first time. Molecular docking experiments showed that all molecules might be able to bind both bitter receptors, providing an excellent basis for applying hop bitter molecules as lead compounds to further design gastrointestinal-permeable T2R agonists
Aglianico grape pomace as a source of antioxidant and anti-proliferative biomolecules: Eco-friendly extraction and HRMS/MS-based molecular networking
Full text linkGrape pomace (GP), a by-product of the wine supply chain process, contains bioactive molecules with known healthy properties. This study examines the impact of different extraction techniques on three GPs of Aglianico cultivar [Cantine del Notaio, Barile, and Torrecuso]. Five eco-friendly extractive techniques [maceration (MAC), digestion (DIG), accelerated solvent extraction (ASE), microwaves (MW), and ultrasound (US)] were used with 50 % ethanol/water as solvent. Spectrophotometric assays showed that DIG and ASE extracts had the highest antioxidant activity and specialized metabolite content. Using the HRMS/MS-based molecular networking, DIG and ASE extract metabolome profiles were analyzed, identifying unknown compounds and known ones with validated antioxidant and chemopreventive effects. In vitro cell-based assay on HepG2 cells demonstrated that Barile GP DIG extract has the highest anti-proliferative activity. Hence, this work provides insight into the potential application of Barile GP DIG extract as a rich source of specialized metabolites with antioxidant and anti-proliferative activity
Pharmacological potential and phytochemical profile of three unexplored medicinal plants
Full text link2017 - 2018Nature is a wide source of biologically active compounds investigated with the
purpose to be used as drugs due to their biological activity and also useful in
pharmaceutical discovery and drug design. Nowadays, medicinal plants play a major role
in primary health care as therapeutic remedies in many developing countries.
The aim of my PhD project was the phytochemical and biological investigation of
three plant species, used in Bolivian traditional medicine, but few scientific studies were
reported, such as: Azorella glabra Wedd., Minthostachys diffusa Epl. and Senecio clivicolus
Wedd.
On the basis of ethnobotanical uses, the samples were firstly analysed for their
total content of polyphenols, flavonoids and terpenoids and for their in vitro antioxidant
activity using different complementary assays. In particular, radical scavenging activity
was tested against biological radicals such as nitric oxide (NO) and superoxide (SO)
together with neutral or cationic (DPPH and ABTS) radicals; ferric reducing power and
lipid peroxidation inhibitory capacity (FRAP and Beta-Carotene Bleaching tests) were also
determined.
Oxidative stress is involved in different diseases, such as diabetes and
neurodegenerative diseases. Then, the inhibitory ability of samples was investigated
against α-amylase and α-glucosidase enzymes involved in diabetes and against
acetylcholinesterase and butyrylcholinesterase enzymes considered as strategy for the
treatment of Parkinson’s or Alzheimer’s diseases.
Moreover, cytotoxicity studies on cancer and non-cancer cell lines were carried
out.
The antioxidant, antidiabetic, anticholinesterase and cytotoxic activities and the
phytochemical profile were performed on aerial parts of A. glabra, M. diffusa and S.
clivicolus for the first time.
Among all samples, the ethyl acetate fraction of S. clivicolus showed the highest
antioxidant activity; instead, M. diffusa samples showed the highest antidiabetic potential
and anti-cholinesterase activities. To confirm the inhibitory cholinesterase effects of the
terpenes identified from M. diffusa, in silico docking analysis were also carried out.
Moreover, the A. glabra samples were tested for the first time on Multiple
Myeloma (MM) cell lines using several assays. The chloroform fraction of A. glabra
reduced the cell viability, and arrested the cell cycle on MM cells in G0/G1 phase,
characteristic feature of apoptosis.
Instead, the ethyl acetate fraction of S. clivicolus was tested on hepatocellular
carcinoma HepG2 cell line showed the ability to induct cell death via the mitochondrial
apoptotic pathway.
In conclusion, this first report on A. glabra, M. diffusa and S. clivicolus
phytochemical characterization and biological activity evaluation, demonstrates as these
Bolivian plant species could be considered a source of health promoting compounds.
Some of the results obtained during this study might partially explain their
ethnobotanical use, evidencing a potential economic added value for extract future use in
the field of biotechnology applied to environmental, agricultural, health, pharmaceutical
and cosmeceutical development. [edited by Author]XXXI cicl
Phenolic Compounds from Olea europaea L. Possess Antioxidant Activity and Inhibit Carbohydrate Metabolizing Enzymes in Vitro
Full text linkPhenolic composition and biological activities of fruit extracts from Italian and Algerian Olea europaea L. cultivars were studied. Total phenolic and tannin contents were quantified in the extracts. Moreover 14 different phenolic compounds were identified, and their profiles showed remarkable quantitative differences among analysed extracts. Moreover antioxidant and enzymatic inhibition activities were studied. Three complementary assays were used to measure their antioxidant activities and consequently Relative Antioxidant Capacity Index (RACI) was used to compare and easily describe obtained results. Results showed that Chemlal, between Algerian cultivars, and Coratina, among Italian ones, had the highest RACI values. On the other hand all extracts and the most abundant phenolics were tested for their efficiency to inhibit α-amylase and α-glucosidase enzymes. Leccino, among all analysed cultivars, and luteolin, among identified phenolic compounds, were found to be the best inhibitors of α-amylase and α-glucosidase enzymes. Results demonstrated that Olea europaea fruit extracts can represent an important natural source with high antioxidant potential and significant α-amylase and α-glucosidase inhibitory effect
Green extractions of bioactives from Vitis vinifera L. (cv. Aglianico) leaves: phenolic profile, antioxidant and anti-cholinesterase activity of extracts.
No full textPreceding researches shown that grape polyphenol compounds defend against oxidative
stress, responsible for neurodegenerative diseases, cancer and diabetes [1, 2]. The aim of this
research is to analyze the effects of several green extraction methods on the quali-quantitative
phenolic profile, on the antioxidant and cholinesterase inhibition activity of Vitis vinifera L.
(cv. Aglianico) leaf extracts
Natural Bioactive Compounds from Orchard Biomass Waste and Cosmetic Applications
Full text linkAntioxidants are crucial in counteracting the impact of free radicals, thereby preventing cell damage. Extracts from orange, apricot, and olive tree pruning, classified as by-products according to environmental laws, underwent examination of their antioxidant properties. In the present investigation, data on the antioxidant activity of extracts of these tree by-products were used to calculate the relative antioxidant capacity index (RACI). The latter made it possible to identify Apricot bark maceration extract as having the highest antioxidant index. Further analysis through UHPLC-MS enabled the identification of compounds known for their antioxidant activity, including catechin, epicatechin, and others. Cytotoxicity assays conducted on human hepatocellular carcinoma cell lines (HepG2) confirmed the safety of the chosen extract for cosmetic applications. The extract was then used to formulate a cosmetic cream, which subsequently underwent quality control and proved to be stable, of good consistency, and free of pathogens. The results show that developing a sustainable cosmetic cream prototype is a promising step toward realizing an environmentally friendly product in the circular economy context
L.)
No full textRecent EU directives have encouraged member states to follow circular economy guidelines on waste reuse, especially for waste originating from wood agro‐forest biomass. Delineating the antioxidant and chemical activity of biomass is a starting point to find new ways to utilize such materials. Here, an 8‐year‐old apricot (Prunus armeniaca L.) tree stand located in southern Italy was evaluated. First, dendrometric parameters (total volume, diameter, and height of trunk below the branches) and physical‐mechanical properties (density, total, tangential and radial shrinkage, moisture content, and compression strength) of timber collected from five experimental plots was evaluated. Bark and wood from apricot pruning were then subjected to different extraction techniques, in vitro antioxidant assays, and gas chromatographic studies to determine their antioxidant activity and their phytochemical composition. Bark had the highest antioxidant activity compared to wood. Several antioxidant compounds (e.g., scopoletin and naringenin) were detected in the samples, explaining the measured antioxidant activity. In conclusion, this study demonstrates the potential of using apricot extracts in nutraceutical, cosmeceutical, and industrial fields
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